CAS:863513-91-1
863513-91-1
CAS号：863513-91-1
品名：Cebranopadol6-fluoro-N,N-dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine
中文别名：Cebranopadol
英文别名：(1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4-b]indole]-4-amine;Cebranopadol;Cebranopadol(USAN/INN);(1r,4r)-6'-fluoro-N,N-dimethyl-4-phenyl-4',9'-dihydro-3'H-spiro[cyclohexane-1,1'-pyrano[3,4-b]indol]-4-amine;
分子式：C24H27FN2O
分子量：378.482
精确质量：378.211
Psa：28.26
密度：1.2±0.1g/cm3
沸点：547.5±50.0°Cat760mmHg
闪点：284.9±30.1°C
折射率：1.644
储存条件：2-8℃
蒸汽压：0.0±1.5mmHgat25°C
简介：Cebranopadol(GRT-6005)isanovelopioidanalgesicofthebenzenoidclasswhichiscurrentlyunderdevelopmentinternationallybyGrünenthal,aGermanpharmaceuticalcompany,anditspartnerDepomed,apharmaceuticalcompanyintheUnitedStates,forthetreatmentofavarietyofdifferentacuteandchronicpainstates.AsofNovember2014,itisinphaseIIIclinicaltrials.Cebranopadolisuniqueinitsmechanismofactionasanopioid,bindingtoandactivatingallfouroftheopioidreceptors;itactsasafullagonistofthenociceptinreceptor(Ki=0.9nM;EC50=13.0;IA=89%),μ-opioidreceptor(Ki=0.7nM;EC50=1.2;IA=104%),andδ-opioidreceptor(Ki=18nM;EC50=110;IA=105%),andasapartialagonistoftheκ-opioidreceptor(Ki=2.6nM;EC50=17;IA=67%).TheED50valuesof0.5-5.6µg/kgwhenintroducedIV&25.1µg/kgafteroraladministration.
G蛋白偶联受体&G蛋白
